A magnetic anti-cancer compound for magnet-guided delivery and magnetic resonance imaging

用于磁导输送和磁共振成像的磁性抗癌化合物

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作者:Haruki Eguchi, Masanari Umemura, Reiko Kurotani, Hidenobu Fukumura, Itaru Sato, Jeong-Hwan Kim, Yujiro Hoshino, Jin Lee, Naoyuki Amemiya, Motohiko Sato, Kunio Hirata, David J Singh, Takatsugu Masuda, Masahiro Yamamoto, Tsutomu Urano, Keiichiro Yoshida, Katsumi Tanigaki, Masaki Yamamoto, Mamoru Sato,

Abstract

Research on controlled drug delivery for cancer chemotherapy has focused mainly on ways to deliver existing anti-cancer drug compounds to specified targets, e.g., by conjugating them with magnetic particles or encapsulating them in micelles. Here, we show that an iron-salen, i.e., μ-oxo N,N'- bis(salicylidene)ethylenediamine iron (Fe(Salen)), but not other metal salen derivatives, intrinsically exhibits both magnetic character and anti-cancer activity. X-Ray crystallographic analysis and first principles calculations based on the measured structure support this. It promoted apoptosis of various cancer cell lines, likely, via production of reactive oxygen species. In mouse leg tumor and tail melanoma models, Fe(Salen) delivery with magnet caused a robust decrease in tumor size, and the accumulation of Fe(Salen) was visualized by magnetic resonance imaging. Fe(Salen) is an anti-cancer compound with magnetic property, which is suitable for drug delivery and imaging. We believe such magnetic anti-cancer drugs have the potential to greatly advance cancer chemotherapy for new theranostics and drug-delivery strategies.

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